Fingolimod (Gilenya)
Sphingosine-1-phosphate (S1P) receptor modulator that sequesters lymphocytes in lymph nodes, reducing CNS-infiltrating autoreactive T cells. First oral disease-modifying therapy approved for relapsing-remitting multiple sclerosis. Dose 0.5 mg PO once daily. Plasma t1/2 ~6-9 days (~144-216h), very long; steady state reached in weeks, with lymphocyte recovery taking 1-2 months after discontinuation. Oral bioavailability ~93%. Metabolized to active fingolimod phosphate by sphingosine kinase; CYP4F2 secondary elimination. FIRST-DOSE CARDIAC OBSERVATION REQUIRED (minimum 6h monitoring for bradycardia/AV block) due to transient S1P1 receptor effect on cardiomyocytes. Risk of macular edema, herpes reactivation, PML (rare), hepatotoxicity, and rebound disease activity on discontinuation.
Projected serum levels — 0.50 mg, once daily
Maintenance schedule: 0.50 mg once daily (oral).
Loading schedule: 1.5 mg on day 1, then 0.50 mg once daily — reaching therapeutic levels sooner.
Modeled steady state after ~20 days: peak ≈ 4.6 mg, trough ≈ 4.4 mg body load. Population-based estimate over 54 days for a 0.50 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.
Key facts
- Category
- Immunosuppressant
- Route modeled
- Oral
- Model confidence
- inferred
- Half-life
- 7 days
- Common dose
- 0.50 mg
- Suggested maximum
- 0.50 mg/day
- Reference dose range
- 0.25–0.50 mg (single dose)
- Suggested cadence
- once daily
- Validated against
- 0.50 mg oral — Cmax 0.002 mg/L at 14 h
Documented interactions
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danger
Levothyroxine (Synthroid) + Fingolimod (Gilenya)
Fingolimod (Gilenya) may displace Levothyroxine (Synthroid) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free…
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warning
Apigenin + Fingolimod (Gilenya)
Apigenin may displace Fingolimod (Gilenya) from plasma protein binding sites, transiently raising free drug concentration.
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warning
Aripiprazole (Abilify) + Fingolimod (Gilenya)
Aripiprazole (Abilify) may displace Fingolimod (Gilenya) from plasma protein binding sites, transiently raising free drug concentration.
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warning
Armour Thyroid (Desiccated Thyroid Extract) + Fingolimod (Gilenya)
Fingolimod (Gilenya) may displace Armour Thyroid (Desiccated Thyroid Extract) from plasma protein binding sites, transiently raising free drug concentration.
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warning
Astaxanthin + Fingolimod (Gilenya)
Astaxanthin may displace Fingolimod (Gilenya) from plasma protein binding sites, transiently raising free drug concentration.
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warning
Atomoxetine (Strattera) + Fingolimod (Gilenya)
Atomoxetine (Strattera) may displace Fingolimod (Gilenya) from plasma protein binding sites, transiently raising free drug concentration.
Serum checks 155 modeled interaction pairings for fingolimod (gilenya) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.
Research behind this entry
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Clinical pharmacokinetics, pharmacodynamics and mechanistic review of fingolimod
Comprehensive PK review: fingolimod F~93%, t1/2 6-9 days, phosphorylated to active fingolimod-P, lymphocyte nadir by day 4 with slow recovery, first-dose HR effect transient.
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A placebo-controlled trial of oral fingolimod in relapsing multiple sclerosis (FREEDOMS)
Pivotal phase 3 RCT: fingolimod 0.5 mg QD reduced annualized relapse rate 54% vs placebo over 24 months in RRMS, first oral DMT approved.
2 published studies referenced in the app, each with a plain-language summary.